1. Field of the invention.
The present invention relates to novel tetralones with pharmacological activity. The invention also relates to a process for their preparation, to pharmaceutical compositions containing them and to their use for the manufacture of medicaments useful in the treatment of mammals, including man. Such tetralones have been found to have blood pressure lowering activity, useful in the treatment of hypertension, as well as bronchodilatory activity, useful in the treatment of asthma. They are also indicated in the treatment of other diseases related with the regulation of the smooth muscle contraction in the gastrointestinal, uterus or urinary tract and in the cardiovascular, respiratory or cerebrovascular systems. Such disorders include angina, congestive heart failure, incontinence, irritable bowel syndrome and epilepsy.
2. Description of the Prior Art.
Several tetralones having antihypertensive activity have been described in the literature, all of them different from the compounds of the present invention.
Our patent applications EP 489300 and EP 525768 disclose certain tetralones with antihypertensive activity of general formula: ##STR2## wherein R.sup.1 and R.sup.2 represent, among others, hydrogen, cyano, nitro, halogen, trifluoromethyl, pentafluoroethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, amino, amino substituted by one or two C.sub.1-4 alkyl groups; R.sup.3 is hydrogen or C.sub.1-4 alkyl; R.sup.4 is C.sub.1-4 alkyl, or R.sup.3 and R.sup.4 together form a C.sub.2-5 polymethylene chain; R.sup.5 is hydroxy or acetoxy and R.sup.6 is hydrogen, or R.sup.5 -R.sup.6 together form a bond; and R.sup.7 represents a cyclic amide or thioamide, saturated or insaturated and optionally substituted, which is bonded to the tetralone ring through the nitrogen atom of the amide moiety, or else R.sup.7 represents a radical --OR.sup.8, wherein R.sup.8 represents certain optionally substituted heterocycles, or R.sup.7 represents an open-chained amine or amide carrying different aliphatic, aromatic or heterocyclic substituents.
The present invention describes new compounds structurally related to the ones described therein, where the nature of the substituent in position 4 of the tetralone ring has been substantially modified.